Pain mechanism

The novel class of pH-dependent NMDA antagonists for pain relief is very interesting (2 June, p 11). You suggest that they may help a subset of patients who do not respond well to treatment with gabapentin. Although gabapentin was originally made to mimic the GABA neurotransmitter, it is now widely believed that its clinical efficacy is a result of modulating voltage-gated calcium channels (namely a2d1 subunits), rather than enhancing the GABA system as stated in your article.

Though there is some controversy over gabapentin's exact mode of action, pharmacological evidence suggests that it does not bind to members of the GABA receptor family nor can its actions be blocked with GABA antagonists. Furthermore, the reduction of a2d1 activity inhibits the release of multiple neurotransmitters (rather than just GABA) within the central nervous system, attenuating the abnormal hyperexcitability observed in neuronal networks in many disorders or conditions, including pain, anxiety and ...

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